Immunity inhibitor glycyrol

An immunosuppressive and immunosuppressive technology, which is applied in the directions of medical preparations containing active ingredients, plant raw materials, organic chemistry, etc. Application and other issues, to achieve the effect of easy modification, small molecular weight and simple structure

Active Publication Date: 2008-08-06
BEIJING NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Commonly used clinical immunosuppressive drugs such as hormones, cyclophosphamide, cyclosporine A, etc., although their curative effects have been prove

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Embodiment 1: the purification of glycyrrhizin

[0015] The dried licorice is crushed to a particle size of 10-20 mesh, put into a percolation device, extracted by ethanol percolation, and the percolation liquid is collected. The percolation liquid was concentrated under reduced pressure and then extracted with ethyl acetate. After the extract was concentrated, the sample was prepared, and then silica gel column chromatography was carried out, and the gradient elution was carried out with petroleum ether-ethyl acetate system, and the fractions were collected, and the solid precipitated fraction was retained . These fractions were purified by high-speed countercurrent chromatography (HSCCC) to obtain white needle-like crystals, and the hydrogen spectrum, carbon spectrum, hydrogen-hydrogen correlation spectrum, carbon-hydrogen correlation spectrum and mass spectrum of the nuclear magnetic resonance spectrum (NMR) The compound was analyzed as glycyrrhizol.

Embodiment 2

[0016] Example 2: Inhibitory effect of Glycyrrhizol on ConA-induced proliferation of mouse T lymphocytes

[0017] The inbred BALB / c mice were sacrificed, the spleen was removed, and the culture medium was used to make cell suspension. Then 100 μl of cell suspension was implanted into a 96-well culture plate, 90 μl of glycyrrhizin of different concentrations was added, and 10 μl of mitogen ConA was added at the same time, and 90 μl of culture solution containing 10% serum was added to the control group. cultured for 72 hours. At the end of the culture, carefully aspirate the supernatant from each well, then add 10 μl MTT, and continue to incubate in the incubator. After 4 hours, add 100 μl of formazan lysate to each well, put it back into the incubator and incubate overnight, and read OD570 on a microplate reader.

[0018] Analysis of the experimental data shows that glycyrrhizin can significantly inhibit the proliferation of T cells induced by ConA (see figure 1 ), and the ...

Embodiment 3

[0019] Example 3: Glycyrrhizol inhibits one-way mixed lymphocyte reaction (MLR):

[0020] Inbred lines BALB / c and C 57 BL mice were sacrificed, spleens were taken, and cell suspensions were made with culture medium. Among them, the inbred strain C 57 Splenocytes from BL mice were treated with mitomycin C as responder cells, splenocytes from inbred BALB / c mice were used as stimulator cells, and the two cell suspensions were mixed in equal volumes. Then, 100 μl of mixed cell suspension and 100 μl of drug solution were added to the 96-well culture plate, and 100 μl of culture solution containing 10% serum was added to the control group, and the two kinds of cells were cultured separately as a control. Incubate for 72 hours at 37°C, 5% carbon dioxide. At the end of the culture, carefully aspirate the supernatant from each well, then add 10 μl MTT, and continue to incubate in the incubator. After 4 hours, add 100 μl of formazan lysate to each well, put it back into the incubato...

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Abstract

A new immunosuppressive agent as glycyrol has significant immunosuppressive activity, thus is useful as an immunosuppressive agent to treat relative diseases, wherein the glycyrol is a coumestrol compound extracted from glycyrrhiza, which is a small molecular compound with novel chemical structure. Tests prove that the glycyrol can inhibit the increment of T lymphocyte induced by canavaline A and inhibit one-way mixed lymphocyte reaction (MLR), release the inflammatory symptom of delayed hypersensitivity and inhibit the homologous allogenic organ transplantation rejection. The glycyrol is a high-effective low-toxicity immunosuppressive agent, with small molecular weight and simple structure, which is easy to be modified and to prepare different drug agents, therefore, the compound is a new generation immunosuppressive agent.

Description

Background technique [0001] Licorice (Glyoyrrhiza uralensis) is the root and rhizome of various plants of the genus Glycyrrhiza Linn in the legume family (Leguminame). The chemical composition of licorice is extremely complex, mainly composed of triterpenoid saponins, flavonoids, coumarins and polysaccharides. The various chemical components of licorice are very important natural active substances, so scholars at home and abroad have conducted in-depth research on the pharmacological activities of licorice extracts and some of their monomers, and have achieved some gratifying results. [0002] Glycyrrhizol (glycyrol) is a class of coumarin compounds in licorice, and there are also reports in China that this compound is new glycyrrhizol (Wang Cailan, Zhang Ruyi, etc., Chemical Research on New Coumarins in Ural Glycyrrhiza, Acta Pharmaceutica Sinica, 1991: 26(2):147-151), scholars at home and abroad have obtained many valuable results in the study of the pharmacological activit...

Claims

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Application Information

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IPC IPC(8): C07D493/04A61K31/37A61P37/06A61K36/484A61K125/00
Inventor 魏群屠颖李家玉骆静吴大伟
Owner BEIJING NORMAL UNIVERSITY
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